Polymer nanoparticle injection formulation composition containing rapamycin with improved water solubility, preparation method thereof, and anticancer composition for combined use with radiotherapy

摘要

The present invention relates to a polymer nanoparticle injection formulation composition containing rapamycin with improved water solubility, and more specifically, to an injection formulation composition containing rapamycin wherein water solubility is improved by solubilizing rapamycin having low water solubility with polymer nanoparticles, a preparation method thereof, and an anticancer composition for a combined use with radiotherapy.

主权项

1. A method for treating cancer in a combination therapy with radiation comprising administering to a subject in need thereof a therapeutically effective amount of an injectable composition comprising polymeric nanoparticles containing rapamycin, wherein the composition comprises:
(i) an A-B type diblock copolymer having a hydrophilic block (A) of methoxy polyethylene glycol and a hydrophobic block (B) of polylactic acid, (ii) an alkali metal salt of polylactic acid or its derivative having at least one carboxyl group on its end, and (iii) rapamycin as an active ingredient, wherein rapamycin is entrapped within the micelle formed from the A-B type diblock copolymer and the alkali metal salt of polylactic acid or its derivative, wherein the composition is reconstituted to the rapamycin concentration of 0.1 to 25 mg/ml, and wherein the composition is administered at the time of, before or after irradiation to mammalian cancer cell to increase a sensitivity of mammalian cancer cell to radiotherapy.